CO6230991A2 - DERIVATIVES OF 3,4-DIHIDRO-1,4-BENZOXAZINE, 3,4-DIHIDRO-1 4-BENZOTIAZINE AND 1,2,3,4-TETRAHYDRO-QUINOXALINE AS AGONISTS OF ALPHA2C ADRENORECEPTORS - Google Patents

DERIVATIVES OF 3,4-DIHIDRO-1,4-BENZOXAZINE, 3,4-DIHIDRO-1 4-BENZOTIAZINE AND 1,2,3,4-TETRAHYDRO-QUINOXALINE AS AGONISTS OF ALPHA2C ADRENORECEPTORS

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Publication number
CO6230991A2
CO6230991A2 CO09084452A CO09084452A CO6230991A2 CO 6230991 A2 CO6230991 A2 CO 6230991A2 CO 09084452 A CO09084452 A CO 09084452A CO 09084452 A CO09084452 A CO 09084452A CO 6230991 A2 CO6230991 A2 CO 6230991A2
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Prior art keywords
dihidro
alkyl
group
halo
alkoxy
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CO09084452A
Other languages
Spanish (es)
Inventor
Kevin D Mccormick
Christopher W Boyce
Neng-Yang Shih
Robert G Aslanian
Salem Fevrier
Pietro Mangiaracina
Lera Ruiz Manuel De
Younong Yu
Junying Zheng
Chia-Yu Huang
Bo Liang
Rong-Quiang Liu
Ruiyan Liu
Lisa Guise-Zawacki
Original Assignee
Schering Corp
Pharmacopeia Llc
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Application filed by Schering Corp, Pharmacopeia Llc filed Critical Schering Corp
Publication of CO6230991A2 publication Critical patent/CO6230991A2/en

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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
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    • C07D279/04—1,3-Thiazines; Hydrogenated 1,3-thiazines
    • C07D279/06—1,3-Thiazines; Hydrogenated 1,3-thiazines not condensed with other rings
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
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    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

Abstract

1.- Un compuesto que tiene la estructura general que se muestra en la Fórmula I:o una sal, éster, solvato o prodroga farmacéuticamente aceptable de dicho compuesto donde: A es un anillo heterocíclico de 5 miembros que contiene 1-3 heteroátomos, y está opcionalmente sustituido con por lo menos un R5 y/o 1 o 2 grupos (=O) (carbonilo); X es -O-, -S(O)p-, o N(R6)-;J1, J2, J3, y J4 son independientemente -N-, -N(O)- o -C(R2)-, con la condición de que 0-3 de J1, J2, J3 y J4 sean -N-; R2 está independientemente seleccionado del grupo que consiste en H, -OH, halo, -CN, -NO2, -S(O)pR7, -NR7R7', -[C(Ra)(Rb)]qYR7', -[C(Ra)(Rb)]qN(R7)YR7´, C(Ra)(Rb)]qOYR7', -[C(Ra)Rb)]qON=CR7R7´, -P(=O)(OR7)(OR7´), -P(=O)NR7R7', y -P(=O)R82, y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo, sustituidos opcionalmente con por lo menos un R5;Y está seleccionado del grupo que consiste en un enlace, -C(=O)-, -C(=O)NR7-, -C(=O)O-, -C(=NR7)-, -C(=O)[C(Ra)(Rb)]n´, -O-C(=O)-, -C(=O)N(Rc)-O-, -C(=NOR7), -C(=NR7)NR7-, -C(=NR7)N(Rc)O, -S(O)p-, -SO2NR7-, y -C(S)NR7-; donde Ra y Rb están independientemente seleccionados del grupo que consiste en H, alquilo, alcoxi, y halo, Rc es H o alquilo; R3 está independientemente seleccionado del grupo que consiste en H, halo, y (=O), y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo, opcionalmente sustituidos con por lo menos un R5, con la condición de que cuando n es 3 o 4, no más de 2 de los grupos R3 pueden ser(=O); R4 está independientemente seleccionado del grupo que consiste en H, -CN, y halo, y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, ...1. A compound having the general structure shown in Formula I: or a pharmaceutically acceptable salt, ester, solvate or prodrug of said compound wherein: A is a 5-membered heterocyclic ring containing 1-3 heteroatoms, and it is optionally substituted with at least one R5 and / or 1 or 2 groups (= O) (carbonyl); X is -O-, -S (O) p-, or N (R6) -; J1, J2, J3, and J4 are independently -N-, -N (O) - or -C (R2) -, with the condition that 0-3 of J1, J2, J3 and J4 be -N-; R2 is independently selected from the group consisting of H, -OH, halo, -CN, -NO2, -S (O) pR7, -NR7R7 ', - [C (Ra) (Rb)] qYR7', - [C ( Ra) (Rb)] qN (R7) YR7´, C (Ra) (Rb)] qOYR7 ', - [C (Ra) Rb)] qON = CR7R7´, -P (= O) (OR7) (OR7´ ), -P (= O) NR7R7 ', and -P (= O) R82, and alkyl, alkoxy, alkenyl, alkenyloxy, alkynyl, cycloalkyl, cycloalkoxy, aryl, aryloxy, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl, and heterocyclyl groups , optionally substituted with at least one R5; Y is selected from the group consisting of a bond, -C (= O) -, -C (= O) NR7-, -C (= O) O-, -C ( = NR7) -, -C (= O) [C (Ra) (Rb)] n´, -OC (= O) -, -C (= O) N (Rc) -O-, -C (= NOR7 ), -C (= NR7) NR7-, -C (= NR7) N (Rc) O, -S (O) p-, -SO2NR7-, and -C (S) NR7-; where Ra and Rb are independently selected from the group consisting of H, alkyl, alkoxy, and halo, Rc is H or alkyl; R3 is independently selected from the group consisting of H, halo, and (= O), and alkyl, alkoxy, alkenyl, alkenyloxy, alkynyl, cycloalkyl, cycloalkoxy, aryl, aryloxy, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl, and heterocyclylalkyl groups, optionally substituted with at least one R5, with the proviso that when n is 3 or 4, no more than 2 of the R3 groups can be (= O); R4 is independently selected from the group consisting of H, -CN, and halo, and alkyl, alkoxy, alkenyl, alkenyloxy, alkynyl, cycloalkyl, cycloalkoxy, aryl, aryloxy, arylalkyl, heteroaryl, ...

CO09084452A 2007-02-13 2009-08-12 DERIVATIVES OF 3,4-DIHIDRO-1,4-BENZOXAZINE, 3,4-DIHIDRO-1 4-BENZOTIAZINE AND 1,2,3,4-TETRAHYDRO-QUINOXALINE AS AGONISTS OF ALPHA2C ADRENORECEPTORS CO6230991A2 (en)

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US (1) US7700592B2 (en)
EP (1) EP2194986A1 (en)
JP (1) JP2010518162A (en)
KR (1) KR20090111345A (en)
CN (1) CN102264369A (en)
AR (1) AR065310A1 (en)
AU (1) AU2008216804A1 (en)
BR (1) BRPI0807911A2 (en)
CA (1) CA2677678A1 (en)
CL (1) CL2008000438A1 (en)
CO (1) CO6230991A2 (en)
EC (1) ECSP099574A (en)
IL (1) IL200337A0 (en)
MX (1) MX2009008773A (en)
PE (1) PE20081782A1 (en)
RU (1) RU2009134061A (en)
TW (1) TW200836746A (en)
WO (1) WO2008100463A1 (en)
ZA (1) ZA200906127B (en)

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